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https://www.readbyqxmd.com/read/28817258/synthesis-of-complex-glycolates-by-enantioconvergent-addition-reactions
#1
Samuel L Bartlett, Jeffrey S Johnson
The unique role that stereochemistry plays in molecular recognition events continues to provide a driving force for synthesizing organic compounds in enantioenriched form. The tendency of enantioenriched organic compounds to revert to an entropically favored racemic state in the presence of viable racemization pathways (e.g., the enolization of stereogenic carbonyl derivatives) can sometimes interfere with this objective; however, beginning with Noyori's foundational disclosure of a dynamic kinetic transfer hydrogenation, the ability to channel racemic, configurationally labile starting materials through stereoconvergent reaction pathways has been recognized as a powerful strategy in asymmetric synthesis...
August 17, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28816044/action-of-gold-nanospikes-based-nanoradiosensitizers-cellular-internalization-radiotherapy-and-autophagy
#2
Ningning Ma, Peidang Liu, Nongyue He, Ning Gu, Fu-Gen Wu, Zhan Chen
A major challenge to achieve effective X-ray radiation therapy is to use a relatively low and safe radiation dose. Various radiosensitizers, which can significantly enhance the radiotherapeutic performance, have been developed. Gold-based nanomaterials, as a new type of nanoparticle-based radiosensitizers, have been extensively used in researches involving cancer radiotherapy. However, the cancer therapeutic effect using the gold nanoparticle-based radiotherapy is usually not significant because of the low cellular uptake efficiency and the autophagy-inducing ability of these gold nanomaterials...
August 17, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28815824/time-of-flight-secondary-ion-mass-spectrometry-tof-sims-using-a-new-primary-ion-beam-generated-by-vacuum-electrospray-of-a-protic-ionic-liquid-propylammonium-nitrate
#3
Yukio Fujiwara, Naoaki Saito
RATIONALE: Protic ionic liquids have the potential to be useful materials for primary ion beams in terms of protonation, since they have active protons. Selecting protic ionic liquids suitable for primary ion beams is of great importance to increase molecular secondary ion yields. Propylammonium nitrate ([C3 H7 NH3 ][NO3 ]) seems promising in view of its proton affinity. It is likely that [C3 H7 NH3 ](+) cations can act as proton donors, and [NO3 ](-) anions can work as proton acceptors...
August 16, 2017: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/28814868/nano-sized-cytochrome-p450-3a4-inhibitors-to-block-hepatic-metabolism-of-docetaxel
#4
Marion Paolini, Laurence Poul, Céline Berjaud, Matthieu Germain, Audrey Darmon, Maxime Bergère, Agnès Pottier, Laurent Levy, Eric Vibert
Most drugs are metabolized by hepatic cytochrome P450 3A4 (CYP3A4), resulting in their reduced bioavailability. In this study, we present the design and evaluation of bio-compatible nanocarriers trapping a natural CYP3A4-inhibiting compound. Our aim in using nanocarriers was to target the natural CYP3A4-inhibiting agent to hepatic CYP3A4 and leave drug-metabolizing enzymes in other organs undisturbed. In the design of such nanocarriers, we took advantage of the nonspecific accumulation of small nanoparticles in the liver...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28814864/controlled-release-of-lovastatin-from-poly-lactic-co-glycolic-acid-nanoparticles-for-direct-pulp-capping-in-rat-teeth
#5
Hung-Pin Lin, Han-Ping Tu, Yu-Ping Hsieh, Bor-Shiunn Lee
Statin at appropriate concentrations has been shown to induce odontoblastic differentiation, dentinogenesis, and angiogenesis. However, using a carrier to control statin release might reduce toxicity and enhance its therapeutic effects. The aim of this study was to prepare poly(d,l-lactide-co-glycolide acid) (PLGA) nanoparticles that contain lovastatin for application in direct pulp capping. The PLGA-lovastatin particle size was determined using dynamic light scattering measurements and transmission electron microscopy...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28814832/combinatorial-and-sequential-delivery-of-gemcitabine-and-oseltamivir-phosphate-from-implantable-poly-d-l-lactic-co-glycolic-acid-cylinders-disables-human-pancreatic-cancer-cell-survival
#6
Stephanie Allison Logan, Amanda J Brissenden, Myron R Szewczuk, Ronald J Neufeld
Combination therapies against multiple targets are currently being developed to prevent resistance to a single chemotherapeutic agent and to extirpate pre-existing resistance in heterogeneous cancer cells in tumors due to selective pressure from the single agent. Gemcitabine (GEM), a chemotherapeutic agent, is the current standard of care for patients with pancreatic cancer. Patients with pancreatic cancer receiving GEM have a low progression-free survival. Given the poor response rate to GEM, cancer cells are known to develop rapid resistance to this drug...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28813539/vectorization-by-nanoparticles-decreases-the-overall-toxicity-of-airborne-pollutants
#7
Rodolphe Carpentier, Anne Platel, Helena Maiz-Gregores, Fabrice Nesslany, Didier Betbeder
Atmospheric pollution is mainly composed of volatile pollutants and particulate matter that strongly interact. However, their specific roles in the induction of cellular toxicity, in particular the impact of the vectorization of atmospheric pollutants by ultrafine particles, remains to be fully elucidated. For this purpose, non-toxic poly-lactic co-glycolic acid (PLGA) nanoparticles were synthesized and three pollutants (benzo(a)pyrene, naphthalene and di-ethyl-hexyl-phthalate) were adsorbed on the surface of the nanoparticles in order to evaluate the toxicity (cytotoxicity, genotoxicity and ROS induction) of these complexes to a human airway epithelial cell line...
2017: PloS One
https://www.readbyqxmd.com/read/28813418/mechanism-of-intracellular-allosteric-%C3%AE-2ar-antagonist-revealed-by-x-ray-crystal-structure
#8
Xiangyu Liu, Seungkirl Ahn, Alem W Kahsai, Kai-Cheng Meng, Naomi R Latorraca, Biswaranjan Pani, A J Venkatakrishnan, Ali Masoudi, William I Weis, Ron O Dror, Xin Chen, Robert J Lefkowitz, Brian K Kobilka
G-protein-coupled receptors (GPCRs) pose challenges for drug discovery efforts because of the high degree of structural homology in the orthosteric pocket, particularly for GPCRs within a single subfamily, such as the nine adrenergic receptors. Allosteric ligands may bind to less-conserved regions of these receptors and therefore are more likely to be selective. Unlike orthosteric ligands, which tonically activate or inhibit signalling, allosteric ligands modulate physiologic responses to hormones and neurotransmitters, and may therefore have fewer adverse effects...
August 16, 2017: Nature
https://www.readbyqxmd.com/read/28809538/dynamic-covalent-hydrogels-for-triggered-cell-capture-and-release
#9
Fatemeh Karimi, Joe Collins, Daniel E Heath, Luke A Connal
A dual-responsive, cell capture and release surface was prepared through the incorporation of phenylboronic acid (PBA) groups into an oxime-based polyethylene glycol (PEG) hydrogel. Owing to its PEG-like properties, the unfunctionalized hydrogel was non-fouling. The use of the highly efficient oxime-click chemistry allows for the facile incorporation of commercially available 3,5-diformylphenyl boronic acid into the hydrogel matrix. Thus, the surface properties of the hydrogel were modified to enable reversible cell capture and release...
August 15, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28809111/tumor-acidic-microenvironment-targeted-drug-delivery-based-on-phlip-modified-mesoporous-organosilica-nanoparticles
#10
Yunlei Zhang, Meng Dang, Ying Tian, Yefei Zhu, Wenfei Liu, Wei Tian, Yunyan Su, Qianqian Ni, Chaoli Xu, Nan Lu, Jun Tao, Yanjun Li, Shuang Zhao, Ying Zhao, Zhenlu Yang, Li Sun, Zhaogang Teng, Guangming Lu
Enhancing the tumor-targeting delivery of chemotherapeutic drugs is important yet challenging for improving therapeutic efficacy and reducing the side effects. Here, we firstly construct a drug delivery system for targeting tumor acidic microenvironment by modification of pH (low) insertion peptide (pHLIP) on mesoporous organosilica nanoparticles (MONs). The MONs has thioether-bridged framework, uniform diameter (60 nm), good biocompatibility and high doxorubicin (DOX) loading capacity (334 mg/g). The DOX loaded in the pHLIP modified MONs can be released responsive to glutathione and low pH circumstance, ensuring the chemotherapeutic drug exerts higher cytotoxic effects to cancer cells than normal cells because of high intracellular GSH of tumor cells and low pH of tumor microenvironment...
August 15, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28809082/development-of-a-dual-functional-hydrogel-using-rgd-and-anti-vegf-aptamer
#11
Nan Zhao, Mark R Battig, Ming Xu, Xiuli Wang, Na Xiong, Yong Wang
Synthetic molecular libraries hold great potential to advance the biomaterial development. However, little effort is made to integrate molecules with molecular recognition abilities selected from different libraries into a single biomolecular material. The purpose of this work is to incorporate peptides and nucleic acid aptamers into a porous hydrogel to develop a dual-functional biomaterial. The data show that an anti-integrin peptide can promote the attachment and growth of endothelial cells in a 3D porous poly(ethylene glycol) hydrogel and an antivascular endothelial growth factor aptamer can sequester and release VEGF of high bioactivity...
August 15, 2017: Macromolecular Bioscience
https://www.readbyqxmd.com/read/28808392/antiurolithiatic-effect-of-sirupeelai-samoola-kudineer-a-polyherbal-siddha-decoction-on-ethylene-glycol-induced-renal-calculus-in-experimental-rats
#12
A Hannah Rachel Vasanthi, V Muthulakshmi, V Gayathri, R Manikandan, S Ananthi, Sarah Kuruvilla
BACKGROUND: Sirupeelai Samoola Kudineer (SK), a polyherbal decoction containing four medicinal plants has been used in Siddha system of medicine, practiced in Southern parts of India for the management of urolithiasis. OBJECTIVE: The present study is carried out to scientifically validate the traditional claim and to study the mechanism of action of the drug. MATERIALS AND METHODS: In the present study, anti-urolithiatic effect of SK was evaluated in Sprague-Dawley rats using ethylene glycol through drinking water and intraperitoneal injection of sodium oxalate...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28808039/preclincial-evaluation-of-intravesical-cisplatin-nanoparticles-for-non-muscle-invasive-bladder-cancer
#13
Max Kates, Abhijit Date, Takahiro Yoshida, Umara Afzal, Pranjali Kanvinde, Taarika Babu, Nikolai A Sopko, Hotaka Matsui, Noah M Hahn, David J McConkey, Alex S Baras, Justin Hanes, Laura Ensign, Trinity J Bivalacqua
PURPOSE: Prior clinical trials evaluating cisplatin for non-muscle invasive bladder cancer (NMIBC) were stopped due to local and systemic toxicity. Currently, there is still a need for improved intravesical therapies, and nanoparticle-based CDDP may be efficacious without the toxicity of free cisplatin observed in the past. EXPERIMENTAL DESIGN: Cisplatin nanoparticles (CDDP NP) were developed using biocompatible poly(L-aspartic acid sodium salt) (PAA), both with and without low and high grafting density of methoxy-polyethylene glycol (PEG)...
August 14, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28805551/bone-targeted-cabazitaxel-nanoparticles-for-metastatic-prostate-cancer-skeletal-lesions-and-pain
#14
Andrew S Gdowski, Amalendu Ranjan, Marjana R Sarker, Jamboor K Vishwanatha
AIM: The aim of this study was to develop a novel cabazitaxel bone targeted nanoparticle (NP) system for improved drug delivery to the bone microenvironment. MATERIALS & METHODS: Nanoparticles were developed using poly(D,L-lactic-co-glycolic acid) and cabazitaxel as the core with amino-bisphosphonate surface conjugation. Optimization of nanoparticle physiochemical properties, in vitro evaluation in prostate cancer cell lines and in vivo testing in an intraosseous model of metastatic prostate cancer was performed...
August 14, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28805228/highly-dispersed-tio2-nanoparticles-with-abundant-active-sites-induced-by-surfactants-as-a-prominent-substrate-for-sers-charge-transfer-contribution
#15
Libin Yang, Di Yin, Yu Shen, Ming Yang, Xiuling Li, Xiaoxia Han, Xin Jiang, Bing Zhao
In this study, highly-dispersed TiO2 nanoparticles (NPs) with abundant active sites were synthesized by a simple sol-hydrothermal method with the assistance of surfactant polyethylene glycol (PEG) which served as an effective SERS-active substrate for the first time. The observed considerable SERS enhancement of 4-mercaptobenzoic acid (4-MBA) probe molecules on TiO2 NPs is attributed to the contribution of the charge transfer mechanism from the substrate to the probe molecule. It is suggested that PEG can act as a protective agent in the reductive calcination of the surfactant-coated nanocrystallite and consequently brings about abundant surface oxygen vacancies for TiO2 NPs, which provide more effective sites for the adsorption of probe molecules and promote the charge transfer effect and its consequent SERS enhancement...
August 14, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28804955/3m-052-as-an-adjuvant-for-a-plga-microparticle-based-leishmania-donovani-recombinant-protein-vaccine
#16
Qian Wang, Meagan A Barry, Christopher A Seid, Elissa M Hudspeth, C Patrick McAtee, Michael J Heffernan
It is believed that an effective vaccine against leishmaniasis will require a T helper type 1 (TH 1) immune response. In this study, we investigated the adjuvanticity of the Toll-like receptor (TLR) 7/8 agonist 3M-052 in combination with the Leishmania donovani 36-kDa nucleoside hydrolase recombinant protein antigen (NH36). NH36 and 3M-052 were encapsulated in separate batches of poly(lactic-co-glycolic acid) (PLGA) microparticles (MPs). The loading efficiency for NH36 was 83% and for 3M-052 was above 95%. In vitro stimulation of bone marrow-derived dendritic cells, measured by IL-12 secretion, demonstrated that 3M-052 (free or MP-formulated) had a concentration-dependent immunostimulatory effect with an optimum concentration of 2 µg/mL...
August 14, 2017: Journal of Biomedical Materials Research. Part B, Applied Biomaterials
https://www.readbyqxmd.com/read/28801269/elastin-plga-hybrid-electrospun-nanofiber-scaffolds-for-salivary-epithelial-cell-self-organization-and-polarization
#17
Zahraa I Foraida, Tim Kamaldinov, Deirdre A Nelson, Melinda Larsen, James Castracane
Development of electrospun nanofibers that mimic the structural, mechanical and biochemical properties of natural extracellular matrices (ECMs) is a promising approach for tissue regeneration. Electrospun fibers of synthetic polymers partially mimic the topography of the ECM, however, their high stiffness, poor hydrophilicity and lack of in vivo-like biochemical cues is not optimal for epithelial cell self-organization and function. In search of a biomimetic scaffold for salivary gland tissue regeneration, we investigated the potential of elastin, an ECM protein, to generate elastin hybrid nanofibers that have favorable physical and biochemical properties for regeneration of the salivary glands...
August 8, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28800875/local-delivery-of-sirna-loaded-calcium-phosphate-nanoparticles-abates-pulmonary-inflammation
#18
Annika Frede, Bernhard Neuhaus, Torben Knuschke, Munisch Wadwa, Sebastian Kollenda, Robert Klopfleisch, Wiebke Hansen, Jan Buer, Dunja Bruder, Matthias Epple, Astrid M Westendorf
The local interference of cytokine signaling mediated by siRNA-loaded nanoparticles might be a promising new therapeutic approach to dampen inflammation during pulmonary diseases. For the local therapeutic treatment of pulmonary inflammation, we produced multi-shell nanoparticles consisting of a calcium phosphate core, coated with siRNAs directed against pro-inflammatory mediators, encapsulated into poly(lactic-co-glycolic acid), and coated with a final outer layer of polyethylenimine. Nasal instillation of nanoparticles loaded with a mixture of siRNAs directed against different cytokines to mice suffering from TH1 cell-mediated lung inflammation, or of siRNA directed against NS-1 in an influenza infection model led to a significant reduction of target gene expression which was accompanied by distinct amelioration of lung inflammation in both models...
August 8, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/28798869/a-novel-akermanite-poly-lactic-co-glycolic-acid-porous-composite-scaffold-fabricated-via-a-solvent-casting-particulate-leaching-method-improved-by-solvent-self-proliferating-process
#19
Yao Deng, Mengjiao Zhang, Xianchun Chen, Ximing Pu, Xiaoming Liao, Zhongbing Huang, Guangfu Yin
Desirable scaffolds for tissue engineering should be biodegradable carriers to supply suitable microenvironments mimicked the extracellular matrices for desired cellular interactions and to provide supports for the formation of new tissues. In this work, a kind of slightly soluble bioactive ceramic akermanite (AKT) powders were aboratively selected and introduced in the PLGA matrix, a novel l-lactide modified AKT/poly (lactic-co-glycolic acid) (m-AKT/PLGA) composite scaffold was fabricated via a solvent casting-particulate leaching method improved by solvent self-proliferating process...
August 2017: Regenerative Biomaterials
https://www.readbyqxmd.com/read/28797972/recent-applications-of-plga-based-nanostructures-in-drug-delivery
#20
REVIEW
Maria Mir, Naveed Ahmed, Asim Ur Rehman
Over the years, issues associated with non-biodegradable polymers have paved the way for biodegradable polymers in the domain of pharmaceutical and biomedical sciences. Poly (lactic-co-glycolic acid) (PLGA) is considered one of the most thrivingly synthesized biodegradable polymers. To formulate polymeric nanostructures, PLGA has attained noteworthy attention due to its controllable properties, complete biodegradability and biocompatibility, well defined formulation techniques and easy processing. This review focuses on fabrication techniques of PLGA based nanostructures and their advanced biomedical applications covering drug delivery and in-vivo imaging...
July 28, 2017: Colloids and Surfaces. B, Biointerfaces
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